Simvastatin-loaded solid lipid nanoparticles for enhanced anti-hyperlipidemic activity in hyperlipidemia animal model

被引：109

作者：

Rizvi, Syed Zaki Husain ^{[1
]}

Shah, Fawad Ali ^{[1
]}

Khan, Namrah ^{[1
]}

Muhammad, Iftikhar ^{[1
]}

Ali, Khan Hashim ^{[1
]}

Ansari, Muhammad Mohsin ^{[1
]}

Din, Fakhar Ud ^{[2
]}

Qureshi, Omer Salman ^{[3
]}

Kim, Kyoung-Won ^{[4
]}

Choe, Yeong-Hwan ^{[4
]}

Kim, Jin-Ki ^{[4
]}

Zeb, Alam ^{[1
]}

机构：

[1] Riphah Int Univ, Riphah Inst Pharmaceut Sci, Sect G-7-4,7th Ave, Islamabad 44000, Pakistan

[2] Quaid I Azam Univ, Dept Pharm, Islamabad, Pakistan

[3] Univ Lahore, Fac Pharm, Lahore, Pakistan

[4] Hanyang Univ, Coll Pharm, Inst Pharmaceut Sci & Technol, 55 Hanyangdaehak Ro, Ansan 15588, Gyeonggi, South Korea

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2019年 / 560卷

基金：

新加坡国家研究基金会;

关键词：

Simvastatin; HMG-CoA reductase; Solid lipid nanoparticles; Sustained release; Hyperlipidemia; Improved therapeutic efficiency; DRUG-DELIVERY SYSTEMS; ORAL DELIVERY; SUSTAINED-RELEASE; BIOAVAILABILITY; CARRIERS; SLN; PHARMACOKINETICS; NANOMEDICINES; OPTIMIZATION; HYPERCHOLESTEROLEMIA;

D O I：

10.1016/j.ijpharm.2019.02.002

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The objective of current study was to develop solid lipid nanoparticles-loaded with simvastatin (SIM-SLNs) and investigate their in vivo anti-hyperlipidemic activity in poloxamer-induced hyperlipidemia model. Nano-template engineering technique was used to prepare SIM-SLNs with palmityl alcohol as lipid core and a mixture of Tween 40/Span 40/Myrj 52 to stabilize the core. The prepared SIM-SLNs were evaluated for physicochemical parameters including particle diameter, surface charge, morphology, incorporation efficiency, thermal behaviour and crystallinity. In vitro release profile of SIM-SLNs in simulated gastric and intestinal fluids was evaluated by using dialysis bag technique and anti-hyperlipidemic activity was assessed in hyperlipidemia rat model. SIMSLNs revealed uniform particle size with spherical morphology, zeta potential of -24.9 mV and high incorporation efficiency (similar to 85%). Thermal behaviour and crystallinity studies demonstrated successful incorporation of SIM in the lipid core and its conversion to amorphous form. SIM-SLNs demonstrated a sustained SIM release from the lipid core of nanoparticles. SIM-SLNs significantly reduced the elevated serum lipids as indicated by similar to 3.9 and similar to 1.5-times decreased total cholesterol compared to those of untreated control and SIM dispersion treated hyperlipidemic rats. In conclusion, SIM-SLNs showed a great promise for improving the therapeutic outcomes of SIM via its effective oral delivery.

引用

页码：136 / 143

页数：8

共 55 条

[51] Improved skin permeation of methotrexate via nanosized ultradeformable liposomes [J].